BDBM104963 CHEMBL507361::US11147816, PD0325901::US11701360, PD0325901::US11964950, Compound Ref-1::US20230270730, Compound ref-1::US8575391, Q
SMILES OC[C@@H](O)CONC(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F
InChI Key InChIKey=SUDAHWBOROXANE-SECBINFHSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 25 hits for monomerid = 104963
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 5.20nMAssay Description:Inhibition assay using MEK kinase.More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 17nMAssay Description:The BRAF-inhibiting activity of the compounds listed in Table 3 below was evaluated by the time-resolved fluorescence-fluorescence resonance energy t...More data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Inhibition of inactive ERK2 (unknown origin) coupled with human MEK1 using IMAP peptide substrate after 30 mins by coupled ERK2 assayMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of activated ERK2 (unknown origin) using IMAP peptide substrate after 30 mins by activated ERK2 assayMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of unphosphorylated ERK2 (unknown origin) by temperature dependent fluorescence (TdF) assayMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 13nMAssay Description:Inhibition of MEK1 (unknown origin) using biotinylated ERK1 as substrate incubated for 2 hrs by fluorescence analysisMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 15nMAssay Description:Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescen...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of N-terminal GST-tagged human BRAF/MEK1/RAF1 Y340D/Y341D double mutant measured after 2 hrs in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataKd: 31nMAssay Description:Binding affinity to MEK1 by surface plasmon resonance in absence of ATPMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataKd: 0.400nMAssay Description:Binding affinity to MEK1 by surface plasmon resonance in presence of ATPMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 8(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 7nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:The test compound, BRAF (Eurofins Genomics KK.) and MEK1 (Thermo Fisher Scientific Inc.) were mixed in ATP-containing buffer and reacted for 90 minut...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 0.600nMAssay Description:Inhibition of MEK1-mediated ERK2 T202/Y204 phosphorylation using biotinylated MBP as substrate preincubated for 30 mins measured after 100 mins by cR...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 15nMAssay Description:Inhibition of recombinant human GST-tagged MEK1 expressed in baculovirus infected Sf9 insect cells using inactive ERK2 as substrate preincubated for ...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Mouse)
University of Michigan
Curated by ChEMBL
University of Michigan
Curated by ChEMBL
Affinity DataIC50: 0.330nMAssay Description:Inhibition of MEK1 in mouse colon 26 cells assessed as reduction in ERK1/2 phosphorylation after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 7nMAssay Description:Inhibition of MEK1 (unknown origin) after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 82nMAssay Description:Inhibition of recombinant full length human His-tagged MEK1 expressed in baculovirus expression system using ERK K52R dead variant as substrate prein...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 2(Human)
Icahn School of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 110nMAssay Description:Inhibition of recombinant full length human His-tagged MEK2 expressed in baculovirus expression system using ERK K52R dead variant as substrate prein...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 13.8nMAssay Description:The IC50 for MEK1 and 2 can be measured by methods in references such as [Yamaguchi et al. (2011) International Journal of Oncology 39:23-31].More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataKd: 44nMAssay Description:Binding affinity to MEK1 (unknown origin) incubated for 1 hr by qPCR based KINOMEscan assayMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 2(Human)
Icahn School of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKd: 100nMAssay Description:Binding affinity to MEK2 (unknown origin) incubated for 1 hr by qPCR based KINOMEscan assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 1(Human)
Chugai Seiyaku Kabushiki Kaisha
US Patent
Chugai Seiyaku Kabushiki Kaisha
US Patent
Affinity DataIC50: 7nMAssay Description:The MEK1-inhibiting activity of the compounds listed in Table 3 below were evaluated by the fluorescent polarization method as described below.The te...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of phosphorylated ERK2 (unknown origin) by temperature dependent fluorescence (TdF) assayMore data for this Ligand-Target Pair